Synthesis and Preliminary Antimicrobial Analysis of Isatin–Ferrocene and Isatin–Ferrocenyl Chalcone Conjugates
Autor: | Vipan Kumar, W.J. Park, Christina C. Tam, Jenny Liu, Kevin Chang, Jihwan Kim, Amandeep Singh, Grant Fong, Kirkwood M. Land, Yun-Hsuan Wu, Luisa W. Cheng |
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Rok vydání: | 2018 |
Předmět: |
0301 basic medicine
Chalcone 010405 organic chemistry General Chemical Engineering Isatin Triazole General Chemistry medicine.disease_cause Antimicrobial 01 natural sciences Combinatorial chemistry Article 0104 chemical sciences lcsh:Chemistry 03 medical and health sciences chemistry.chemical_compound 030104 developmental biology lcsh:QD1-999 chemistry medicine Trichomonas vaginalis Growth inhibition IC50 Pathogen |
Zdroj: | ACS Omega, Vol 3, Iss 5, Pp 5808-5813 (2018) ACS Omega |
ISSN: | 2470-1343 |
DOI: | 10.1021/acsomega.8b00553 |
Popis: | In this study, we outline the synthesis of isatin–ferrocenyl chalcone and 1H-1,2,3-triazole-tethered isatin–ferrocene conjugates along with their antimicrobial evaluation against the human mucosal pathogen Trichomonas vaginalis. The introduction of a triazole ring among the synthesized conjugates improved the activity profiles with most of the compounds in the library, exhibiting 100% growth inhibition in a preliminary susceptibility screen at 100 μM. IC50 determination of the most potent compounds in the set revealed an inhibitory range between 2 and 13 μM. Normal flora microbiome are unaffected by these compounds, suggesting that these may be new chemical scaffolds for the discovery of new drugs against trichomonad infections. |
Databáze: | OpenAIRE |
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